Positional Scanning Peptide Libraries for Kinase Substrate Specificity Determinations: Straightforward and Reproducible Synthesis Using Pentafluorophenyl Esters.
Artikel i vetenskaplig tidskrift, 2010

An efficient method to synthesize positional scanning synthetic combinatorial libraries (PS-SCLs) for studying the specificity of protein kinases is presented. Isokinetic ratios for pentafluorophenyl esters were determined iteratively using a new approach incorporating high performance liquid chromatography (HPLC) quantification and statistical experimental design. In the development process a large amount of work was put in to find efficient ways of screening for new isokinetic mixtures and to optimize the process of PS-SCL synthesis. The newly developed methods for the screening of isokinetic mixtures could be used for the screening of other interesting mixtures, but more importantly, the isokinetic ratios determined for the preactivated pentafluorophenyl esters were incorporated into a new efficient protocol. This straightforward protocol allows for a convenient synthesis of high quality PS-SCLs regardless of previous experience in solid phase synthesis.

Författare

Thomas Ljungdahl

Göteborgs universitet

Jenny Veide Vilg

Göteborgs universitet

Fredrik Wallner

Göteborgs universitet

Markus J. Tamás

Göteborgs universitet

Morten Grøtli

Göteborgs universitet

Journal of Combinatorial Chemistry

1520-4766 (ISSN) 1520-4774 (eISSN)

Vol. 12 733-742

Ämneskategorier

Organisk kemi

DOI

10.1021/cc100095y

PubMed

20608733